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April 15, 2020 / / - Human infection with Severe Acute Respiratory Syndrome (SARS-CoV-2) can lead to coronavirus disease (COVID-19), there is no cure.
class 3c protease (3CLpro) is a highly conservative protease essential for coronavirus replication and a promising target for the development of broad-spectrum antiviral drugs.
In order to speed up the discovery and development of drugs, researchers from the Shanghai Institute of Pharmaceutical Research, the University of Chinese Academy of Sciences, the Chinese University of Pharmacy, Shanghai University of Science and Technology and other units studied the inhibition of SARS-CoV-2 3CLpro from natural products of Chinese medicine. natural product resenceors of SARS-CoV-2 3CL protease in vitro".
photo source: BioRxiv researchers have for the first time found non-co-priced, non-peptide SARS-CoV-2 3CLpro inhibitors - jaundice and jaundice.
researchers found in cell experiments that the two components showed strong antiviral activity in the cellular system.
note that the combination of jaundice and SARS-CoV-2 3CLpro as measured by x-ray protein crystallology is significantly different from known inhibitors.
Jaundice is perfectly fixed at the center of the substrate binding point through interaction with two catalytic residuals (critical S1/S2 substops and oxygen anion rings) and acts as a "shield" before catalyzing the binary, preventing the peptide substrate from approaching the active point.
Overall, the simple chemical structure, unique mode of action and strong in-body antiviral activity, coupled with good clinical trial safety data, provide a great opportunity to develop jaundice as a much-needed anti-coronavirus drug.
() Reference: Haixia Su et al. Discovery of baicalin and baicalein as novel, natural product product resedors of SARS-CoV-2 3CL protease in vitro. bioRxiv. 2020. doi: https://doi.org/10.1101/2020.04.13.038687.